Soticlestat

• CAT Number: I036516
• CAS Number: 1429505-03-2
• Molecular Formula: C23H23N3O2
• Molecular Weight: 373.45
• Purity: ≥95%
• Synonyms: (4-benzyl-4-hydroxypiperidin-1-yl)-(2-pyridin-4-ylpyridin-3-yl)methanone
• InChI: InChI=1S/C23H23N3O2/c27-22(20-7-4-12-25-21(20)19-8-13-24-14-9-19)26-15-10-23(28,11-16-26)17-18-5-2-1-3-6-18/h1-9,12-14,28H,10-11,15-17H2
• InChIKey: XKUZMIUSBMCVPP-UHFFFAOYSA-N
• SMILES: C1CN(CCC1(CC2=CC=CC=C2)O)C(=O)C3=C(N=CC=C3)C4=CC=NC=C4

Soticlestat (TAK-935; OV935) is a first-in-class, potent, selective, and orally active cholesterol 24-hydroxylase (CH24H) inhibitor. Soticlestat has the potential for epilepsy syndromes research[1][2].
Soticlestat inhibits the catalytic activity of human cholesterol 24-hydroxylase (CH24H) in a concentration-dependent manner with an IC50 of 4.5 nM[1].
Soticlestat treatment lowers brain 24S-hydroxycholesterol in a dose-dependent manner and substantially reduceds premature deaths of APP/PS1-Tg mice at a dose lowering brain 24S-hydroxycholesterol by approximately 50%. Soticlestat can suppress potassium-evoked extracellular glutamate elevations in the hippocampus[1].

Reference

[1]. Toshiya Nishi, et al. Soticlestat, a novel cholesterol 24-hydroxylase inhibitor shows a therapeutic potential for neural hyperexcitation in mice. Sci Rep. 2020 Oct 13;10(1):17081.
 [Content Brief]

[2]. Krista Eschbach, et al. Stiripentol for the treatment of seizures in Dravet syndrome. Expert Rev Clin Pharmacol. 2019 May;12(5):379-388.
 [Content Brief]